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BH3I-1 inhibits Bcl-xL heterodimerization in vitro. It also induces cytochrome c release. BH3I-1, while inhibiting its reported target Bcl-2/Bim and Bcl-xL/Bim, shows significant inhibition of both the p53/hDM2 and p300/Hif-1a interactions. BH3I-1 inhibits interaction between the BH3 domain and Bcl-xL. NMR analyses reveal that BH3I-1 targets the BH3-binding pocket of Bcl-xL with a Ki of 7.8±0.9 μM.
| Cell Experiment | |
|---|---|
| Cell lines | Jurkat cells |
| Preparation method | Cells (5×10^4 cells per well) are seeded into white 96-well plates (Costar) and treated with various concentrations of the compounds for 48 h. For zVAD-FMK protection experiments, cells are preincubated with 100 µM zVAD-FMK for 1 h before the addition of chemicals. Cell viability is determined with an MTS assay. For PI staining experiments, cells are grown in 24-well plates and then incubated with 2 µg ml/L PI. Cell death is determined by FACS analysis. |
| Concentrations | 30 or 90 μM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 400.31 |
| Formula | C15H14BrNO3S2 |
| CAS Number | 300817-68-9 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Bcl-2 Products |
|---|
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| ABT-737
ABT-737 is a potent and selective inhibitor of B-cell lymphoma-2 (BCL-2) family proteins, in small cell lung cancer. |
| AT-101
AT-101 (R-(-)-gossypol acetic acid) is a pan small molecule inhibitor of Bcl-2, Bcl-xL, and Mcl-1. |
| ABT-199
ABT-199 (Venetoclax) is a highly potent, orally bioavailable and BCL-2 inhibitor. ABT-199 is the first inhibitor targeting Bcl-2 and PPI. |
| TW-37
TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively. |
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